Quinoline Ligands for Pd catalyzed C-H activation


Pd catalyzed C-H activation is a powerful method for installing functional groups onto biologically relevant molecules. However, C(sp3)-H activation has proven quite challenging. Ligand selection is critical for these types of transformations because the ligands tune the metal catalyst’s reactivity and selectivity. Quinoline derived ligands (ALD0004 and ALD00002), developed in Jin-Quan Yu’s lab, have proven to be the most effective ligands for promoting C(sp3)-H activation thus far.


The Yu Lab has demonstrated a variety of transformations using the quinoline derived ligands. For example, the Li-Yu t-Butyl quinoline is optimal for γ-C(sp3)-H functionalization such as, olefination, arylation, and alkylation. 


Representative Application

Additionally, the Li-Yu quinoline promotes C-H activation of methylene bonds and enables arylation of secondary β–C(sp3)-H bonds for the sequential installation of aryl groups. It has successfully been utilized in the synthesis of β-Aryl-α-amino acids.



To learn more about other products in our catalog that have been established in collaboration with Professor Yu, please visit his Professor Product Page.

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